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( Lijun Wei ),( Nirmal Marasini ),( Gao Li ),( Chul Soon Yong ),( Jong Oh Kim ),( Qizhe Quan ) 영남대학교 약품개발연구소 2013 영남대학교 약품개발연구소 연구업적집 Vol.23 No.0
Ligustrazine is a traditional Chinese medicine used to treat various cardiovascular and neurovascular complications. However, this compound exhibits rapid first-pass metabolism, a short biological half-life, low stability and potential vascular irritation that restrict its use for long-term therapy. The use of a lipid emulsion as a carrier for intravenous administration of ligustrazine might provide sustained and prolonged release, thereby reducing the frequency of administration and improving patient compliance. The main purpose of our study was to develop a highly stable and sterile optimal formulation of a ligustrazine lipid emulsion (LLE) and to evaluate its pharmacokinetic behavior and tissue distribution in rats. The final optimal formulation consisted of soybean oil (12.0%), oleic acid (0.6%), lecithin (1.0%), poloxamer 188 (0.6%) and glycerol (2.25%). The average particle size, polydispersity index (PDI), zeta-potential and pH of the final product were 215.0±2.5 nm, 0.076±0.033, -40.4±5.3 mV and 7.25±0.05, respectively. The LLE was stable for at least three months at room temperature. In vitro drug release studies of the LLE suggested a sustained release profile, which was further confirmed by in vivo pharmacokinetic studies in rats. The area under the drug concentration-time curve from 0 h to 10 h (AUC(0-10h)) for LLE was increased by 1.6-fold compared with that of the commercially available ligustrazine injection (LI), suggesting enhanced bioavailability from the lipid-based emulsion. Furthermore, a tissue distribution study showed significant improvement in the distribution pattern of ligustrazine with a higher AUC(0-180 min) observed in all tissues for LLE than for LI. In conclusion, LLE, with excellent stability, improved pharmacokinetics and tissue distribution, demonstrates great potential for the delivery of ligustrazine for clinical applications.ⓒ2012 Elsevier B.V.All rights reserved.
Lipid Emulsion as a Drug Delivery System for Breviscapine: Formulation Development and Optimization
Wei, Lijun,Li, Gao,Yan, Yi-Dong,Pradhan, Roshan,Kim, Jong Oh,Quan, Qizhe 대한약학회 2012 Archives of Pharmacal Research Vol.35 No.6
In this study, we developed an optimized formulation of a breviscapine lipid emulsion (BLE) and evaluated the physicochemical properties and in vivo pharmacokinetics of BLE in rats. For the preparation of the lipid emulsion, soybean oil and oleic acid were used as the oil phase, lecithin and poloxamer 188 as surfactants and glycerol as co-surfactant. An optimized formulation consisting of soybean oil (10.0%), oleic acid (0.9%), lecithin (1.5%), poloxamer 188 (0.4%), and glycerol (2.25%) was selected. The results showed that the average particle size, polydispersity index, and zeta potential of the optimized formulation were $183.5{\pm}5.5$ nm, $0.098{\pm}0.046$, and $-35.0{\pm}2.5$ mV, respectively. The BLE was stable for at least three month at room temperature. After a single intravenous dose of 4 mg/kg to rats, the AUC of scutellarin from the lipid emulsion was about 1.5-fold higher than that of the commercial product (breviscapine injection). In conclusion, the optimized formulation of BLE showed positive results over the commercial product in terms of the physicochemical properties and pharmacokinetics of BLE in rats.
Lipid Emulsion as a Drug Delivery System for Breviscapine: Formulation Development and Optimization
Lijun Wei,Qizhe Quan,Gao Li,Yi-Dong Yan,Roshan Pradhan,김종오 대한약학회 2012 Archives of Pharmacal Research Vol.35 No.6
In this study, we developed an optimized formulation of a breviscapine lipid emulsion (BLE) and evaluated the physicochemical properties and in vivo pharmacokinetics of BLE in rats. For the preparation of the lipid emulsion, soybean oil and oleic acid were used as the oil phase, lecithin and poloxamer 188 as surfactants and glycerol as co-surfactant. An optimized formulation consisting of soybean oil (10.0%), oleic acid (0.9%), lecithin (1.5%), poloxamer 188 (0.4%), and glycerol (2.25%) was selected. The results showed that the average particle size, polydispersity index, and zeta potential of the optimized formulation were 183.5 ± 5.5 nm, 0.098 ± 0.046, and −35.0 ± 2.5 mV, respectively. The BLE was stable for at least three month at room temperature. After a single intravenous dose of 4 mg/kg to rats, the AUC of scutellarin from the lipid emulsion was about 1.5-fold higher than that of the commercial product (breviscapine injection). In conclusion, the optimized formulation of BLE showed positive results over the commercial product in terms of the physicochemical properties and pharmacokinetics of BLE in rats.
Novel Ceramides from Aerial Parts of Saussurea involucrata Kar. et. Kir.
Wei Wu,Yang Qu,Huiyuan Gao,Jingyu Yang,Jianguo Xu,Lijun Wu 대한약학회 2009 Archives of Pharmacal Research Vol.32 No.9
Novel ceramides, together with nine known compounds were isolated from aerial parts of the Saussurea involucrata Kar. et. Kir. The novel structures were determined by spectroscopic methods and microscale chemical degradation. The ceramides showed appreciable cytotoxicity against three human tumor cell lines including human promyelocytic leukemia (HL-60), human melanoma (A375-S2) and human cervical carcinoma (HeLa) cell lines. The results suggested that this class of ceramides may have potential as an antitumor agent.
Effect of Nd ion on the magnetic properties of Ni-Mn ferrite nanocrystal
Lijun Zhao,Wei Xu,Hua Yang,Lianxiang Yu 한국물리학회 2008 Current Applied Physics Vol.8 No.1
The nanocrystalline Ni0.7Mn 0.3Nd 0.1Fe1.9O4 ferrites were prepared by the emulsion method. X-ray diractometer (XRD), transmis-sion electron microscope (TEM), Mo¨ssbauer spectra and vibrating samples magnetometer (VSM) were used to study the structure, mor-phology and magnetic properties. The magnetic properties of Nd3+-doped Ni0.7Mn 0.3Fe2O4 nanocrystal ferrites were investigated indetail. The Ni0.7Mn 0.3Nd 0.1Fe1.9O4 nanocrystal ferrite with particle size of 10.7 nm shows superparamagnetism.
Active Fault-tolerant Control Design for a Submarine Semi-physical Simulation System
Lijun Liu,Wei Yu,Zhen Yu 제어·로봇·시스템학회 2018 International Journal of Control, Automation, and Vol.16 No.5
In this paper, an integrated design of fault diagnosis and active fault-tolerant control is proposed for a submarine semi-physical simulation system in the presence of unknown faults of rudder systems. The semi-physical simulation system is constructed by combining two real rudder control systems and a virtual mathematical model for the vertical movement control of a submarine. The separate modules of the semi-physical simulation system are connected by industrial communication technologies. Then, an active fault-tolerant controller is designed for unknown rudder system faults. Finally, the results of the semi-physical simulation experiments verify the effectiveness of the proposed fault-tolerant control method, and make a solid foundation for designing an active fault-tolerant control system for a real submarine.
Lijun Tang,Raju Nandhakumar,Gongfan Wei,Zhilong Guo 대한화학회 2011 Bulletin of the Korean Chemical Society Vol.32 No.9
An easy and convenient synthetic route to (S)-2-hydroxy-2'-(3-phenyluryl-benzyl)-1,1'-binaphthyl-3-carboxaldehyde (1), capable of recognizing tryptophan by fluorescence has been developed. The binol carboxaldehyde 1 exhibited a high selectivity to L-tryptophan over other examined L-α-amino acids such as alanine,phenylalanine, glutamine, arginine, lysine, serine, threonine, aspartat, valine, histidine and cysteine, with a fluorescence “turn-on” signal. In addition, 1 displayed chiral discrimination with good enantioselectivity toward L-tryptophan over D-tryptophan through different fluorescence enhancement factors.
Wu Wei,Zhang Xiaxiang,Yang Jianxiao,Lijun Cai,Li Xuanke 한국탄소학회 2020 Carbon Letters Vol.30 No.6
The oxygen-rich activated carbon (AC) was facilely developed using petroleum coke as a raw material by KOH activa�tion under the rapid heating rate. The porosity and surface chemistry of ACs prepared under diferent heating rates were characterized and their adsorption properties for methylene blue (MB) were investigated. The results showed that the AC5 prepared under the heating rate of 5 °C min−1 had the highest surface area compared with the AC10, AC15 or AC20, while the AC20 prepared under the heating rate of 20 °C min−1 consisted of the highest oxygen content and most –OH functional group compares with the other ACs. These indicated that rapid heating rate was against the formation of more developed porosity, however, it was benefcial to producing more oxygen functional groups. As to MB adsorption, AC15 exhibited the maximum adsorption capacity for MB of 884 mg g−1 due to high surface area of 2803 m2 g−1 and high oxygen content of 23.27%. Moreover, despite the fact that AC20 had much lower surface area than the AC5, the AC20 showed higher MB adsorption capacity than the AC5. This was because the AC20 has the highest content of –OH, which was a positive impetus for MB adsorption. Therefore, rapid heating rate was an efective and simple approach to preparing the oxygen-rich ACs for improving the adsorption capacity of MB.
Tang, Lijun,Wei, Gongfan,Nandhakumar, Raju,Guo, Zhilong Korean Chemical Society 2011 Bulletin of the Korean Chemical Society Vol.32 No.9
An easy and convenient synthetic route to (S)-2-hydroxy-2'-(3-phenyluryl-benzyl)-1,1'-binaphthyl-3-carboxaldehyde (1), capable of recognizing tryptophan by fluorescence has been developed. The binol carboxaldehyde 1 exhibited a high selectivity to L-tryptophan over other examined L-${\alpha}$-amino acids such as alanine, phenylalanine, glutamine, arginine, lysine, serine, threonine, aspartat, valine, histidine and cysteine, with a fluorescence "turn-on" signal. In addition, 1 displayed chiral discrimination with good enantioselectivity toward L-tryptophan over D-tryptophan through different fluorescence enhancement factors.